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Melatonin and Its Agonists in Sleep Disorders

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Melatonin and Melatonergic Drugs in Clinical Practice

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Abstract

Exogenous melatonin reportedly induces drowsiness and sleep and may ameliorate sleep disturbances, including the nocturnal awakenings associated with old age. Daytime administration of exogenous melatonin (when it is not present endogenously) promotes sleep in humans and results in sleeplike brain activity patterns at specific areas such as the precuneus and hippocampus. However, existing studies on the hypnotic efficacy of melatonin have been highly heterogeneous in regard to inclusion and exclusion criteria, measures to evaluate insomnia, doses of the medication, and routes of administration.

The inconsistent reports about the effectiveness of exogenous melatonin in the treatment of insomnia brought about the development of more potent melatonin analogs with prolonged effects and the design of slow-release melatonin preparations. The melatonergic receptor ramelteon is a selective melatonin-1 (MT1) and melatonin-2 (MT2) receptor agonist with negligible affinity for other neuronal receptors, including gamma-aminobutyric acid and benzodiazepine receptors. It was found effective in increasing total sleep time and sleep efficiency as well as in reducing sleep latency, in insomnia patients. The melatonergic antidepressant agomelatine, displaying potent MT1 and MT2 melatonergic agonism and relatively weak serotonin 5-HT2C receptor antagonism, reportedly is effective in the treatment of depression-associated insomnia. A review of the currently available evidence regarding the effects of these compounds on sleep quality is presented in this chapter.

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Authors and Affiliations

  1. Department of Obstetrics and Gynecology, Hadassah Hebrew-University Medical Center, Ein-Kerem, Jerusalem, 91120, Israel

    Amnon Brzezinski MD

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  1. Amnon Brzezinski MD
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Correspondence to Amnon Brzezinski MD .

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Editors and Affiliations

  1. Sri Sathya Sai Medical Educational and Research Foundation, An International Medical Sciences Research Center, Coimbatore, Tamil Nadu, India

    V. Srinivasan

  2. Department of Obstetrics and Gynecology, Hadassah Hebrew-University Medical Center, Jerusalem, Israel

    Amnon Brzezinski

  3. Department of Physiology, Gulhane Military Medical Academy, Ankara, Turkey

    Sukru Oter

  4. Department of Psychiatry Behavioral Sciences, Mercer University School of Medicine, Macon, Georgia, USA

    Samuel D. Shillcutt

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Brzezinski, A. (2014). Melatonin and Its Agonists in Sleep Disorders. In: Srinivasan, V., Brzezinski, A., Oter, S., Shillcutt, S. (eds) Melatonin and Melatonergic Drugs in Clinical Practice. Springer, New Delhi. https://doi.org/10.1007/978-81-322-0825-9_18

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